公开(公告)号：US20120214759A1

公开(公告)日：2012-08-23

申请号：US13294426

申请日：2011-11-11

申请人： Jon B. Bruss ,  George H. Miller ,  James Bradley Aggen ,  Eliana Saxon Armstrong

发明人： Jon B. Bruss ,  George H. Miller ,  James Bradley Aggen ,  Eliana Saxon Armstrong

IPC分类号： A61K31/7028 ,  A61P31/04

CPC分类号： A61K31/7036 ,  A61K31/706 ,  Y02A50/473 ,  Y02A50/483

摘要： A method for treating a Klebsiella pneumonia infection in a mammal in need thereof is disclosed, the method comprising administering to the mammal an effective amount of an antibacterial aminoglycoside compound.

摘要翻译： 公开了用于治疗有需要的哺乳动物感染肺炎克雷伯杆菌的方法，该方法包括向哺乳动物施用有效量的抗菌氨基糖苷类化合物。

公开(公告)号：US07838665B2

公开(公告)日：2010-11-23

申请号：US11874548

申请日：2007-10-18

申请人： Eliana Saxon ,  Carolyn Ruth Bertozzi

发明人： Eliana Saxon ,  Carolyn Ruth Bertozzi

IPC分类号： C07H5/06

CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

摘要翻译： 本发明的特征在于可以在生理条件下进行的化学选择性连接反应。 通常，本发明涉及特异性改造的膦的缩合，其可以提供在两个反应性配对物之间形成酰胺键，产生包含膦部分的最终产物，或者可被工程化以包含可切割连接体，使得 将膦的取代基转移到叠氮化物中，释放氧化的膦副产物并在最终产物中产生天然酰胺键。 反应的选择性及其与水性环境的相容性在体内（例如，在细胞表面或细胞内）和体外（例如，肽和其他聚合物的合成，修饰（例如，标记的）氨基酸的产生 ）。

公开(公告)号：US07635598B2

公开(公告)日：2009-12-22

申请号：US11177998

申请日：2005-07-08

申请人： Ronald M. Cook ,  Eliana Saxon Armstrong ,  Hans E. Johansson

发明人： Ronald M. Cook ,  Eliana Saxon Armstrong ,  Hans E. Johansson

IPC分类号： G01N33/533 ,  G01N33/53 ,  C12Q1/26 ,  C12N1/21 ,  C12P21/00

CPC分类号： C12Q1/26 ,  C09B11/08 ,  C12Q1/6818 ,  C12Q1/6897 ,  G01N33/542 ,  G01N2333/90209 ,  Y10S436/903 ,  Y10T436/13

摘要： In one aspect, the invention provides fluorescent probes and assays. The probes include a fluorophore-quencher pair that undergoes a switch from dark to fluorescent in response to a reaction of the quencher. The switch of the probe from dark to fluorescent is typically mediated by an enzyme that acts directly or indirectly on the quencher, interfering with its ability to quench fluorescence emission from the fluorophore.In another aspect, the invention provides a reporter gene assay system and methods of using this system. The assay system includes a fluorophore-quencher probe and an enzyme that acts directly or indirectly on the quencher, increasing the fluorescent emission of the fluorophore. In still other aspects, the invention provides nucleic acid constructs and cells expressing the peptide products of these constructs.In assays of the invention, the presence of a target substance is detected by the switching of fluorescence mediated by the change in oxidation state of the quencher. The assay systems are of use in numerous assay formats, e.g., confirming the expression of the enzyme that acts on the quencher, and/or detecting a species conjugated to the enzyme.

摘要翻译： 一方面，本发明提供了荧光探针和测定法。 探针包括响应于猝灭剂的反应经历从暗变为荧光的荧光团 - 猝灭剂对。 探针从黑暗到荧光的切换通常由直接或间接作用于猝灭剂的酶介导，干扰其从荧光团中淬灭荧光发射的能力。 另一方面，本发明提供报道基因测定系统和使用该系统的方法。 测定系统包括荧光团猝灭剂探针和直接或间接作用于猝灭剂的酶，增加荧光团的荧光发射。 在其它方面，本发明提供了表达这些构建体的肽产物的核酸构建体和细胞。 在本发明的测定中，通过由猝灭剂的氧化态的变化介导的荧光的转换来检测目标物质的存在。 测定系统可用于许多测定形式，例如确认作用于猝灭剂的酶的表达和/或检测与酶缀合的物质。

公开(公告)号：US20090220982A1

公开(公告)日：2009-09-03

申请号：US12392035

申请日：2009-02-24

申请人： Eliana Saxon Armstrong ,  Lee Ann Feeney ,  Corwin F. Kostrub

发明人： Eliana Saxon Armstrong ,  Lee Ann Feeney ,  Corwin F. Kostrub

IPC分类号： C12Q1/02 ,  C12Q1/34 ,  C12Q1/26 ,  C12Q1/68

CPC分类号： G01N33/5044 ,  G01N33/5014 ,  G01N2800/347

摘要： The present invention provides novel in vitro assays for determining the nephrotoxicity of a compound. These assays correlate well with in vivo nephrotoxicity and also provide high-throughput methods to screen multiple compounds for in vivo nephrotoxicity. In addition, the methods of the present invention may be adapted to screen for nephroprotectant compounds, including those that protect cells and animals from the nephrotoxic effects of aminoglycoside antibiotics.

摘要翻译： 本发明提供用于测定化合物的肾毒性的新型体外测定法。 这些测定与体内肾毒性良好相关，并且还提供高通量的方法筛选多种化合物用于体内肾毒性。 此外，本发明的方法可以适用于筛选肾脏保护剂化合物，包括保护细胞和动物免受氨基糖苷类抗生素的肾毒性作用的化合物。

公开(公告)号：US06570040B2

公开(公告)日：2003-05-27

申请号：US09810864

申请日：2001-03-16

申请人： Eliana Saxon ,  Carolyn Bertozzi

发明人： Eliana Saxon ,  Carolyn Bertozzi

IPC分类号： C12N502

CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

公开(公告)号：US08076496B2

公开(公告)日：2011-12-13

申请号：US13043274

申请日：2011-03-08

申请人： Eliana Saxon ,  Carolyn Ruth Bertozzi

发明人： Eliana Saxon ,  Carolyn Ruth Bertozzi

IPC分类号： C07C247/00 ,  C07C233/00 ,  G01N33/53

CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

公开(公告)号：US07923582B2

公开(公告)日：2011-04-12

申请号：US11039478

申请日：2005-01-19

申请人： Eliana Saxon ,  Carolyn R. Bertozzi

发明人： Eliana Saxon ,  Carolyn R. Bertozzi

IPC分类号： C07F9/02 ,  C07C205/00

CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

摘要翻译： 本发明的特征在于可以在生理条件下进行的化学选择性连接反应。 通常，本发明涉及特异性改造的膦的缩合，其可以提供在两个反应性配对物之间形成酰胺键，产生包含膦部分的最终产物，或者可被工程化以包含可切割连接体，使得 将膦的取代基转移到叠氮化物中，释放氧化的膦副产物并在最终产物中产生天然酰胺键。 反应的选择性及其与水性环境的相容性在体内（例如，在细胞表面或细胞内）和体外（例如，肽和其他聚合物的合成，修饰（例如，标记的）氨基酸的产生 ）。

公开(公告)号：US07667012B2

公开(公告)日：2010-02-23

申请号：US11408605

申请日：2006-04-20

申请人： Eliana Saxon ,  Carolyn R. Bertozzi

发明人： Eliana Saxon ,  Carolyn R. Bertozzi

IPC分类号： A61K31/7008 ,  C07H5/04 ,  C07H5/06

CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g. on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

摘要翻译： 本发明的特征在于可以在生理条件下进行的化学选择性连接反应。 通常，本发明涉及特异性改造的膦的缩合，其可以提供在两个反应性配对物之间形成酰胺键，产生包含膦部分的最终产物，或者可被工程化以包含可切割连接体，使得 将膦的取代基转移到叠氮化物中，释放氧化的膦副产物并在最终产物中产生天然酰胺键。 反应的选择性及其与水性环境的相容性使其在体内（例如在细胞表面或细胞内）和体外（例如肽和其它聚合物的合成，修饰（例如，标记的）氨基酸的生产） 。

公开(公告)号：US20050148032A1

公开(公告)日：2005-07-07

申请号：US11039478

申请日：2005-01-19

申请人： Eliana Saxon ,  Carolyn Bertozzi

发明人： Eliana Saxon ,  Carolyn Bertozzi

IPC分类号： C07F9/50 ,  C07F9/6506 ,  C07F9/655 ,  C07F9/6561 ,  C07K1/02 ,  C07K1/04 ,  C07K1/107 ,  C12N5/02 ,  G01N33/53 ,  G01N33/567 ,  C12Q1/68 ,  C07F9/22 ,  C07C247/16

CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

摘要翻译： 本发明的特征在于可以在生理条件下进行的化学选择性连接反应。 通常，本发明涉及特异性改造的膦的缩合，其可以提供在两个反应性配对物之间形成酰胺键，产生包含膦部分的最终产物，或者可被工程化以包含可切割连接体，使得 将膦的取代基转移到叠氮化物中，释放氧化的膦副产物并在最终产物中产生天然酰胺键。 反应的选择性及其与水性环境的相容性在体内（例如，在细胞表面或细胞内）和体外（例如，肽和其他聚合物的合成，修饰（例如，标记的）氨基酸的产生 ）。